Conantokins, peptides from Conus snails, are N-methyl-d-aspartate (NMDA) receptor antagonists. NMDA receptor antagonists potentiate l-3,4-dihydroxyphenylalanine (l-DOPA)-induced rotation in 6-hydroxydopamine-treated rodents, an index of anti-Parkinsonian potential. This study examined the effect...
Preliminary studies using the dog indicated that the highly potent analgesic etorphine is relatively much more effective than morphine, after sublingual administration. Experiments using tritium labelled materials showed that this difference between the drugs could probably be explained by the f...
A sensitive and specific method was developed for the determination of dihydrocodeine and its metabolite dihydromorphine in human serum using codeine and morphine as internal standards. Measurement is performed with GC-tandem MS after one simple extraction step and derivatization to the pentaflu...
A high-performance liquid chromatography assay for the oxidative metabolites of dihydrocodeine, nordihydrocodeine and dihydromorphine, formed in human liver microsomal incubations, is described. A simple solvent extraction followed by reversed-phase high-performance liquid chromatography with UV...
These studies demonstrated that 5-ethyl-5-(3-hydroxyl-1-methyl-butyl)-barbituric acid (PB-OH), a major metabolite of pentobarbital, antagonized pentobarbital-induced narcosis in both naive and pentobarbital tolerant mice. In PB-OH pretreated mice, the sleeping time induced by sodium pentobarbita...
Publisher SummaryThis chapter focuses on the resolution of racemic α-amino acids. When same proteins are hydrolyzed by an alkaline agent, such as strong baryta, amino acids are optically inactive and posses different solubilities from those of the corresponding active forms. These values are ob...
The plasma levels of deoxycorticosterone sulfate (DOC-SO4) in near-term pregnant women are ∼100 times those in plasma of men or non-pregnant women. Yet, neither the tissue site of synthesis nor the precursor of DOC-SO4 that enters maternal plasma is known. Several potential sources have been ex...
The activity of steroid 21-sulfatase, the enzyme that catalyzes the hydrolysis of deoxycorticosterone sulfate (DOC-SO4) is demonstrable in human placenta. Thus, it is possible that this placental enzyme, by way of the hydrolysis of either DOC-SO4 or 21-hydroxypregnenolone mono- or di-sulfate of ...
The present investigation was conducted to evaluate the potential for the transfer of deoxycorticosterone (DOC) and deoxycorticosterone sulfate (DOC-SO4) from the fetal to the maternal compartment in near-term human pregnancy. To do so we measured progesterone, DOC, and DOC-SO4 in maternal venou...
The concentrations of progesterone, deoxycorticosterone (DOC), and deoxycorticosterone sulfate (DOC-SO4) were determined in mixed umbilical cord plasma of abortuses and newborn infants delivered between 18 and 42 weeks' gestation. A wide range of values among individual samples was found fo...
In the present investigation, we determined the metabolic clearance rate of plasma deoxycorticosterone sulfate in adult men and nonpregnant women and in one woman pregnant at 42 weeks gestation with an anencephalic fetus. The values obtained varied from 618 to 1070 l/24 h. The metabolic clearanc...
SummaryEthanol and the neuroactive steroids have interactive neuropharmacological effects and chronic ethanol administration blunts the ethanol-induced increase in neuroactive steroid levels in rodent plasma and brain. Few studies have explored neuroactive steroid regulation in alcohol-dependent...
In the present investigation, we determined the levels of deoxycorticosterone sulfate in mixed umbilical cord plasma of anencephalic abortuses and newborn infants. The anencephalic fetus is an interesting model with respect to the production of deoxycorticosterone and deoxycorticosterone sulfate...
The hapten of deoxycorticosterone sulfate was synthesized and linked to the carrier protein through the C-4 position on the steroid nucleus. The antisera raised against this antigen in guinea pigs exhibited high affinity (Ka=1.86 × 109 M−1) and excellent specificity for deoxycorticosterone sulf...
SUMMARYOf approximately 3,500 recovery room patients, 5 per cent vomited one or more times. Either thiethylperazine or placebo was then administered in double-blind style, and both agents were approximately 60 per cent successful after one injection. However, 56 per cent of a similar series of (...
A double-blind trial was undertaken to compare thiethylperazine (Torecan) and pyridoxine as anti-emetics in patients undergoing externally applied radiotherapy to the abdomen and pelvis. The patients who received thiethylperazine experienced fewer or much milder symptoms than those given pyridoxine.
The results of the study presented here corroborate the findings of previous investigations that thiethylperazine is a very useful and dependable antiemetic agent. The onset of action is rapid, and no side effects or incidents of extrapyramidal reaction were observed at any time throughout the s...
The synthesis of thiethylperazine (= Torecan®) with a 35S-labelled phenothiazine ring is described. Its resorption, distribution in the organism, and its excretion in the faeces, urine and bile are investigated in the rat and compared with similar investigations for thioridazine.
The effects of cinnarizine, sulpiride, thiethylperazine and a placebo on vestibular nystagmus in rabbits were investigated. The nystagmus was provoked by means of a torsion swing. A suppressive effect was shown by all drugs and not by the placebo. A fast and strong effect was seen after the admi...
Dystonic reactions in 30 children receiving thiethylperazine are reported. All children developed extrapyramidal symptoms following therapeutic or excess dose of the drug. All these symptoms were effectively reversed with biperidine lactate.
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